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1. 发明授权

US12109219B2 Cannabinoid receptor modulators 有权
公开(公告)号：US12109219B2
公开(公告)日：2024-10-08
申请号：US16849216
申请日：2020-04-15
申请人： Arena Pharmaceuticals, Inc.
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06
CPC分类号： A61K31/675 , A61K31/416 , A61K31/4439 , A61K31/497 , A61K45/06 , A61K31/416 , A61K2300/00
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

2. 发明授权

US11780827B2 Substituted 3-phenoxyazetidin-1-yl-pyrazines 有权
公开(公告)号：US11780827B2
公开(公告)日：2023-10-10
申请号：US17215759
申请日：2021-03-29
申请人： Boehringer Ingelheim International GmbH , Arena Pharmaceuticals, Inc.
发明人： Kai Gerlach , Graeme Semple , Yifeng Xiong , Barbara Bertani , Marco Ferrara , Giacomo Fossati , Scott Hobson , Uta Friederike Lessel , Frank Runge , Ursula Mueller-Vieira , Julian Wippich
IPC分类号： C07D403/14
CPC分类号： C07D403/14
摘要： The invention relates to substituted 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) which are agonists of GPR52, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) for use as a medicament, pharmaceutical compositions comprising the 3-phenoxyazetidin-1-yl-pyrazines of general formula (I) and processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention.

3. 发明申请

US20170151236A1 IMIDAZO[1,2-A]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
公开(公告)号：US20170151236A1
公开(公告)日：2017-06-01
申请号：US15400670
申请日：2017-01-06
申请人： Arena Pharmaceuticals, Inc.
发明人： Yifeng Xiong , Konrad Feichtinger , Albert S. Ren , Brett Ulmann
IPC分类号： A61K31/496 , A61K9/00 , A61K31/5377
CPC分类号： A61K31/496 , A61K9/0019 , A61K9/0053 , A61K31/5377 , C07D471/04
摘要： Imidazo[1,2-a]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

4. 发明授权

US11771695B2 Cannabinoid receptor modulators 有权
公开(公告)号：US11771695B2
公开(公告)日：2023-10-03
申请号：US17478274
申请日：2021-09-17
申请人： Arena Pharmaceuticals, Inc.
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/497 , C07D231/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07F9/6558 , A61K31/416 , A61K31/4439 , A61K31/675 , A61K45/06 , A61K31/13 , A61K31/485
CPC分类号： A61K31/497 , A61K31/13 , A61K31/416 , A61K31/4439 , A61K31/485 , A61K31/675 , A61K45/06 , C07D231/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/14 , C07F9/65583
摘要： Provided are certain methods useful in the treatment of pain comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

5. 发明申请

US20210060040A1 CANNABINOID RECEPTOR MODULATORS 有权
公开(公告)号：US20210060040A1
公开(公告)日：2021-03-04
申请号：US16849216
申请日：2020-04-15
申请人： Arena Pharmaceuticals, Inc.
发明人： Jayant Thatte , Anthony C. Blackburn , Sangdon Han , Robert M. Jones , Jae-Kyu Jung , Antonio Garrido Montalban , Biman B. Pal , Jaimie Karyn Rueter , Sonja Strah-Pleynet , Lars Thoresen , Yifeng Xiong , Dawei Yue , Xiuwen Zhu
IPC分类号： A61K31/675 , A61K31/416 , A61K45/06 , A61K31/4439 , A61K31/497
摘要： Provided are certain methods useful in the treatment of cancer comprising administering a compound of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor;

6. 发明授权

US10781180B2 3-phenyl-pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 有权
公开(公告)号：US10781180B2
公开(公告)日：2020-09-22
申请号：US16177672
申请日：2018-11-01
申请人： Arena Pharmaceuticals, Inc.
发明人： Bradley Teegarden , Yifeng Xiong , Sonja Strah-Pleynet , Honnappa Jayakumar , Peter I. Dosa , Konrad Feichtinger , Martin Casper , Juerg Lehmann , Robert M. Jones , David J. Unett , Jin Sun Karoline Choi
IPC分类号： C07D401/12 , C07D403/12 , C07D231/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D487/08 , C07D231/16 , C07D417/12 , A61K31/5377 , C07D413/10
摘要： The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

7. 发明申请

US20180354907A1 CANNABINOID RECEPTOR MODULATORS 审中-公开
公开(公告)号：US20180354907A1
公开(公告)日：2018-12-13
申请号：US15912700
申请日：2018-03-06
申请人： Arena Pharmaceuticals, Inc.
发明人： Robert M. Jones , Sangdon Han , Lars Thoresen , Jae-Kyu Jung , Sonja Strah-Pleynet , Xiuwen Zhu , Yifeng Xiong , Dawei Yue
IPC分类号： C07D231/54 , C07D403/04 , C07D413/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07F9/6558 , C07D403/12 , C07D405/14 , C07D413/12
CPC分类号： C07D231/54 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07F9/65583
摘要： The present invention relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor. The present invention further relates to certain compounds of Formula Ia and pharmaceutical compositions thereof that modulate the activities of both the CB1 receptor and the CB2 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of: pain, for example bone and joint pain, muscle pain, dental pain, migraine and other headache pain, inflammatory pain, neuropathic pain, pain that occurs as an adverse effect of therapeutics and pain associated with osteoarthritis; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation; atherosclerosis; undesired immune cell activity and inflammation; age-related macular degeneration; cough; leukemia; lymphoma; CNS tumors; prostate cancer; Alzheimer's disease; stroke-induced damage; dementia; amyotrophic lateral sclerosis, and Parkinson's disease.

8. 发明申请

US20170320831A1 PYRAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
公开(公告)号：US20170320831A1
公开(公告)日：2017-11-09
申请号：US15657896
申请日：2017-07-24
申请人： Arena Pharmaceuticals, Inc.
发明人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
IPC分类号： C07D231/16 , C07D403/14 , C07D403/12 , C07D403/06 , C07D231/54 , C07D405/04 , C07D231/14
CPC分类号： C07D231/16 , C07D231/14 , C07D231/54 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

9. 发明授权

US09732039B2 Pyrazole derivatives as modulators of the 5-HT2A serotonin receptor useful for the treatment of disorders related thereto 有权
公开(公告)号：US09732039B2
公开(公告)日：2017-08-15
申请号：US14692807
申请日：2015-04-22
申请人： Arena Pharmaceuticals, Inc.
发明人： Yifeng Xiong , Martin C. Cherrier , Jin Sun Karoline Choi , Peter I. Dosa , Brian M. Smith , Sonja Strah-Pleynet , Brett Ullman , Bradley Teegarden
IPC分类号： C07D231/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D231/16 , C07D231/54 , C07D403/14
CPC分类号： C07D231/16 , C07D231/14 , C07D231/54 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04
摘要： Pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT2A receptor. Formula (Ia). Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.

10. 发明申请

US20160318911A1 1-HETEROARYL-INDOLINE-4-CARBOXAMIDES AS MODULATORS OF GPR52 USEFUL FOR THE TREATMENT OR PREVENTION OF DISORDERS RELATED THERETO 有权
标题翻译：作为GPR52调节剂的1-HETEROARYL-INDOLINE-4-CARBOXAMIDES可用于治疗或预防相关疾病
公开(公告)号：US20160318911A1
公开(公告)日：2016-11-03
申请号：US15143026
申请日：2016-04-29
申请人： Arena Pharmaceuticals, Inc.
发明人： Yifeng Xiong , Andrew J. Grottick , Henry Korman , Juerg Lehmann , Albert S. Ren , Graeme Semple
IPC分类号： C07D405/14 , C07D403/04 , C07D401/14 , C07D401/04
CPC分类号： C07D405/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/14
摘要： The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of GPR52. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a GPR52-mediated disorder (e.g., Huntington's disease, schizophrenia, bipolar disorder, attention deficit hyperactivity disorder (ADHD), or Tourette's syndrome); an extrapyramidal or movement disorder; a motor disorder; a hyperkinetic movement disorder; a psychotic disorder; catatonia; a mood disorder; a depressive disorder; an anxiety disorder; obsessive-compulsive disorder (OCD); an autism spectrum disorder; a prolactin-related disorder (e.g., hyperprolactinemia); a neurocognitive disorder; a trauma- or stressor-related disorder (e.g., posttraumatic stress disorder (PTSD)); a disruptive, impulse-control, or conduct disorder; a sleep-wake disorder; a substance-related disorder; an addictive disorder; a behavioral disorder; hypofrontality; an abnormality in the tuberoinfundibular, mesolimbic, mesocortical, or nigrostriatal pathway; decreased activity in the striatum; cortical dysfunction; neurocognitive dysfunction; and conditions related thereto
摘要翻译：本发明涉及调节GPR52活性的式（Ia）化合物及其药物组合物。本发明的化合物及其药物组合物涉及可用于治疗GPR52介导的病症（例如亨廷顿氏病，精神分裂症，双相情感障碍，注意缺陷多动障碍（ADHD）或图雷特综合征）的方法）。锥体外系或运动障碍; 运动障碍运动障碍; 精神障碍紧张症; 情绪障碍抑郁障碍焦虑症强迫症（OCD）; 自闭症谱系障碍催乳素相关病症（例如高催乳素血症）; 神经认知障碍创伤或压力相关障碍（如创伤后应激障碍（PTSD））; 破坏性，冲动控制或行为障碍; 睡眠障碍物质相关疾病; 成瘾性障碍行为障碍次方数结节性下颌，中脑边缘，中皮质或黑质纹状体通路异常; 纹状体活动减少; 皮质功能障碍神经认知功能障碍和相关条件

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